Givinostat (ITF-2357) is an HDAC inhibitor with IC50s of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat (ITF-2357) decreases surface CXCR4 and CCR5 expression on CD4(+) T-cells and monocytes and is superior to valproic acid for latent HIV-1 expression in vitro. Givinostat reduces cytokines and protects islet β cells in vivo and in vitro. Treatment with Givinostat ≥500 nM is associated with significant inhibition of JS-1 cell proliferation (P<0.01). Also, the cell inhibition rate significantly differs between the group cotreated with Givinostat ≥250 nM plus LPS and the group without LPS treatment (same Givinostat concentration) (P<0.05).
| Cell Experiment | |
|---|---|
| Cell lines | JS-1 cells |
| Preparation method | JS-1 cell line is cultured in DMEM with 10% fetal bovine serum for 24 h, 30 wells of JS-1 cells are divided into two groups. In the first group, the culture medium is replaced by complete medium with final Givinostat (ITF-2357) concentrations of 0 nM, 125 nM, 250 nM, 500 nM, and 1000 nM. In the second group, Givinostat of relevant concentrations is added concomitantly with 100 nM of LPS solution. Three replicates are performed for each group. After inoculation at 37°C and 5% CO2 for 24 h, each well (100 μL) is incubated with 10 μL of CCK-8 solution. The plates are incubated at 37°C for 1 h and the absorbance is measured at 450 nm using a microplate reader. |
| Concentrations | 0 nM, 125 nM, 250 nM, 500 nM, and 1000 nM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | C57BL/6 mice |
| Formulation | |
| Dosages | 10 mg/kg |
| Administration | orally |
| Molecular Weight | 421.49 |
| Formula | C24H27N3O4 |
| CAS Number | 497833-27-9 |
| Solubility (25°C) | DMSO ≥ 100 mg/mL |
| Storage | Powder -20°C |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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